Identification
- Summary
Porfimer sodium is a hematoporphyrin derivative used to treat esophageal cancer, endobronchial cancer, and high grade dysplasia in Barrett's Esophagus.
- Brand Names
- Photofrin
- Generic Name
- Porfimer sodium
- DrugBank Accession Number
- DB00707
- Background
The purified component of hematoporphyrin derivative, it consists of a mixture of oligomeric porphyrins. It is used in photodynamic therapy (hematoporphyrin photoradiation); to treat malignant lesions with visible light and experimentally as an antiviral agent. It is the first drug to be approved in the use of photodynamic therapy in the United States.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Porfimer natrium
- Porfimer sodico
- Porfimer sodium
- Porfimère sodique
- Porfimerum natricum
Pharmacology
- Indication
Indicated in the treatment of esophageal cancer.
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- Contraindications & Blackbox Warnings
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Porfimer is a photosensitizing agent used in the photodynamic therapy (PDT) of tumors. Porfimer is indicated for the palliation of patients with completely obstructing esophageal cancer, or of patients with partially obstructing esophageal cancer who cannot be satisfactorily treated with Nd:YAG laser therapy, reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial nonsmall cell lung cancer (NSCLC), and the treatment of microinvasive endobronchial NSCLC in patients for whom surgery and radiotherapy are not indicated. The cytotoxic and antitumor actions of porfimer are light and oxygen dependent. Tumor selectivity in treatment occurs through a combination of selective retention of porfimer and selective delivery of light.
- Mechanism of action
Cellular damage caused by porfimer is a consequence of the propagation of radical reactions. Radical initiation may occur after porfimer absorbs light to form a porphyrin excited state. Spin transfer from porfimer to molecular oxygen may then generate singlet oxygen. Subsequent radical reactions can form superoxide and hydroxyl radicals. Tumor death also occurs through ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by thromboxane A2 release.
Target Actions Organism ULow-density lipoprotein receptor other/unknownHumans UHigh affinity immunoglobulin gamma Fc receptor I antagonistHumans - Absorption
Not Available
- Volume of distribution
- 0.49 ± 0.28 L/kg [2 mg/kg dose of porfimer sodium to 4 male cancer patients]
- Protein binding
~90%
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
10-452 hours
- Clearance
- Renal cl=199.7 +/- 56.9 mL/min [Healthy subjects receiving a single 300-mg oral dose]
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAminolevulinic acid Aminolevulinic acid may increase the photosensitizing activities of Porfimer sodium. Articaine The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Articaine. Benzocaine The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Benzocaine. Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Benzyl alcohol. Bupivacaine The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Bupivacaine. Butacaine The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Butacaine. Butamben The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Butamben. Capsaicin The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Capsaicin. Carprofen Carprofen may increase the photosensitizing activities of Porfimer sodium. Chloroprocaine The risk or severity of methemoglobinemia can be increased when Porfimer sodium is combined with Chloroprocaine. 
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- No interactions found.
Products
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- PhotoBarr (Axcan) / Photofrin II
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Photofrin Powder, for solution 15 mg / vial Intravenous Concordia Pharmaceuticals, Inc 1995-12-31 2014-11-21 Canada 
Photofrin Injection, powder, for solution 75 mg/31.8mL Intravenous Pinnacle Biologics, Inc. 1995-12-27 Not applicable US 
Photofrin Powder, for solution 75 mg / vial Intravenous Concordia Pharmaceuticals, Inc 1995-12-31 2019-07-18 Canada Photofrin Injection, powder, for solution 2.5 mg/1mL Intravenous Axcan Scandipharm Inc. 2006-09-11 Not applicable US
Categories
- ATC Codes
- L01XD01 — Porfimer sodium
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Biological Factors
- Dermatologicals
- Hematoporphyrin Derivative
- Hematoporphyrins
- Heterocyclic Compounds, Fused-Ring
- Photoabsorption
- Photoactivated Radical Generator
- Photosensitizing Activity
- Photosensitizing Agents
- Photosensitizing Agents for Phototherapy
- Pigments, Biological
- Porphyrins
- Radiation-Sensitizing Agents
- Sensitizers Used in Photodynamic/radiation Therapy
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- Y3834SIK5F
- CAS number
- 87806-31-3
References
- General References
- Not Available
- External Links
- PubChem Substance
- 46508600
- ChemSpider
- 10482043
- 333848
- ChEBI
- 60652
- PharmGKB
- PA164752658
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Porfimer_sodium
- FDA label
- Download (321 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Axcan pharma us inc
- Packagers
- Axcan Pharma Inc.
- Draxis Specialty Pharmaceuticals Inc.
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 2.5 mg/1mL Injection, powder, for solution Intravenous 75 mg/31.8mL Powder, for solution Intravenous Powder, for solution Intravenous 15 mg / vial Powder, for solution Intravenous 75 mg / vial - Prices
Unit description Cost Unit Photofrin 75 mg vial 3317.04USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5145863 No 1992-09-08 2009-12-15 US CA2094974 No 1996-10-22 2013-04-27 Canada
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 2.8 Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Virus receptor activity
- Specific Function
- Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clat...
- Gene Name
- LDLR
- Uniprot ID
- P01130
- Uniprot Name
- Low-density lipoprotein receptor
- Molecular Weight
- 95375.105 Da
References
- Korbelik M: Low density lipoprotein receptor pathway in the delivery of Photofrin: how much is it relevant for selective accumulation of the photosensitizer in tumors? J Photochem Photobiol B. 1992 Jan;12(1):107-9. [Article]
- Tsukagoshi S: [Porfimer sodium (Photofrin-II)]. Gan To Kagaku Ryoho. 1995 Aug;22(9):1271-8. [Article]
- Maziere JC, Mora L, Biade S, Maziere C, Santus R: [Potentiation of the photocytotoxic effect of photofrin II: synergistic action of verapamil and lovastatin]. Bull Acad Natl Med. 1994 Jun;178(6):1177-88; discussion 1188-9. [Article]
- Candide C, Morliere P, Maziere JC, Goldstein S, Santus R, Dubertret L, Reyftmann JP, Polonovski J: In vitro interaction of the photoactive anticancer porphyrin derivative photofrin II with low density lipoprotein, and its delivery to cultured human fibroblasts. FEBS Lett. 1986 Oct 20;207(1):133-8. [Article]
- Maziere JC, Morliere P, Biade S, Santus R: [Antitumor photochemotherapy: biochemical bases, therapeutic uses and perspectives]. C R Seances Soc Biol Fil. 1992;186(1-2):88-106. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor signaling protein activity
- Specific Function
- High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
- Gene Name
- FCGR1A
- Uniprot ID
- P12314
- Uniprot Name
- High affinity immunoglobulin gamma Fc receptor I
- Molecular Weight
- 42631.525 Da
References
- Krutmann J, Athar M, Mendel DB, Khan IU, Guyre PM, Mukhtar H, Elmets CA: Inhibition of the high affinity Fc receptor (Fc gamma RI) on human monocytes by porphyrin photosensitization is highly specific and mediated by the generation of superoxide radicals. J Biol Chem. 1989 Jul 5;264(19):11407-13. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 27, 2022 18:28